紫苏叶提取物乳膏剂的处方研究

Ointment formulation optimization of extracts from Perilla frutescens

中药紫苏叶中富含黄酮类有效成分,外用之后具有抗氧化以及促进表皮细胞生长等生理活性。本研究采用"新生皂法"将紫苏叶醇提物制备成水包油(O/W)型乳膏剂,并通过正交设计对处方中影响乳膏成型性的因素进行了筛选,得到性质稳定、肤感良好的制剂。利用超声提取法对紫苏叶中的黄酮类组分进行提取,以外观均一性、涂布延展性、离心稳定性及耐寒耐热性的综合评分作为考察指标,对油相/水相质量比例、三乙醇胺用量以及辅助乳化剂单硬脂酸甘油酯用量进行正交设计,以筛选出乳膏剂的最优处方。优选处方下,油相/水相比例为35∶65,三乙醇胺和单硬脂酸甘油酯的质量百分比分别为0.6%和3%。制备得到的水包油(O/W)型乳膏剂稳定性良好,为后期进一步应用奠定了基础。

Flavonoids and other effective components are abundant in extracts from leaves of Perilla frutescens with bioactivitiesof anti-oxidant and promoting epidermal cell growth through transdermal administration. Aiming at these characteristics,ointment was prepared for extracts from leaves of Perilla frutescens with oil-in-water（O/W）type through nascent soap method.Meanwhile, orthogonal screening was used in formulation selection in order to obtain stable ointment formulation with preferredskin-feeling. In this investigation, flavonoid ingredients were acquired through ultrasonic extraction firstly. Afterwards,comprehensive scoring of homogeneity, extensibility, centrifugal stability and cold/heat resistance was set as the evaluationindicator to obtain the optimal ratio of oil phase/water phase, triethanolamine and coemulsifier-glycerin monostearate. Afterprepared under the optimal formulation, in which the ratio of oil phase/water phase was 35：65, and the mass percentage oftriethanolamine and glycerin monostearate was 0.6% and 3%（m/m）respectively, stable ointment was acquired in oil-in-watertype. This study provided the basis for further application of Perilla frutescens extracts ointment.